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Abilify

Abilify
The drug Abilify® solution for intramuscular administration is used to quickly relieve the state of arousal and behavioral disorders in patients with schizophrenia and in patients with manic episodes with bipolar I disorder when the drug cannot be taken orally.

Brand: Aripiprazole

Availability: In Stock
Average Delivery Time: 9 Days
Exp. Date: November 2023
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Abilify 20 mg
270 pills - 20 mg
+ 12 free Viagra 100 mg, 7% discount for future orders
$350.99 $1.30 $350.56 Add to cart
180 pills - 20 mg
+ 8 free Viagra 100 mg, 5% discount for future orders
$248.95 $1.38 $218.75 Add to cart
120 pills - 20 mg
+ 4 free Viagra 100 mg, 3% discount for future orders
$180.35 $1.50 $131.45 Add to cart
90 pills - 20 mg
+ 4 free Viagra 100 mg, 3% discount for future orders
$146.21 $1.62 $87.64 Add to cart
60 pills - 20 mg
+ 4 free Viagra 100 mg, 3% discount for future orders
$112.53 $1.88 $43.37 Add to cart
30 pills - 20 mg $77.95 $2.60 No Add to cart
Abilify 15 mg
270 pills - 15 mg
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$219.86 $0.81 $211.69 Add to cart
180 pills - 15 mg
+ 4 free Viagra 100 mg, 3% discount for future orders
$155.75 $0.87 $131.95 Add to cart
120 pills - 15 mg
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$112.95 $0.94 $78.85 Add to cart
90 pills - 15 mg $90.79 $1.01 $53.06 Add to cart
60 pills - 15 mg $70.99 $1.18 $24.91 Add to cart
30 pills - 15 mg $47.95 $1.60 No Add to cart
Abilify 10 mg
270 pills - 10 mg
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$178.95 $0.66 $77.24 Add to cart
180 pills - 10 mg
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$126.91 $0.71 $43.88 Add to cart
90 pills - 10 mg $73.91 $0.82 $11.49 Add to cart
60 pills - 10 mg $56.93 $0.95 No Add to cart
Abilify 5 mg
270 pills - 5 mg
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$135.55 $0.50 $57.73 Add to cart
180 pills - 5 mg $95.55 $0.53 $33.30 Add to cart
120 pills - 5 mg $68.99 $0.57 $16.91 Add to cart
90 pills - 5 mg $55.85 $0.62 $8.58 Add to cart
60 pills - 5 mg $42.95 $0.72 No Add to cart

Product description

Pharmacological action of Abilify

INN means - aripiprazole. The therapeutic effect of aripiprazole in schizophrenia is determined by the combination of selective agonistic action against D2 dopamine and 5HT1a serotonin receptors and antagonistic activity against 5HT2 serotonin terminals. 

Picture of the packaging of the drug Abilify

Aripiprazole has good in vitro affinity for the D2 and D3 dopamine terminals. The active substance is also characterized by an average affinity for the sites of reuptake of the hormone of happiness and a lack of affinity for the muscarinic endings. In experiments on animals, it showed opposition in relation to dopaminergic overactivity and agonism in relation to dopaminergic inactivity. Some clinical effects of aripiprazole can be explained by the relationship not only with dopamine and serotonin endings. 

Pharmacodynamics of the drug The

activity of the drug Abilify is determined by the presence of the active ingredient - aripiprazole. The half-life is 75 hours. A stable concentration is noted after 2 weeks. The accumulation of medication with repeated use is predictable. No daily fluctuations in the distribution of the substance and its metabolite dehydroaripiprazole were observed. 

Packing of tablets Abilify

The active ingredient is promptly absorbed after the use of Abilify. The maximum permissible concentration is noted after 3-5 hours. Full bioavailability is 87%. Eating food does not affect the bioavailability of aripiprazole. 

The substance is distributed in tissues. At a therapeutic concentration of more than 99%, aripiprazole binds to serum proteins especially with albumin. Aripiprazole has no effect on the pharmacokinetics and pharmacodynamics of warfarin. 

The active substance undergoes presystemic decay to the least extent. Aripiprazole is the main component of the drug in the blood. After a single application, 27 and 60% are detected in urine and feces. 

Indications for use 

Use of Abilify for schizophrenia

Indications for use of Abilify:

  • schizophrenia: supportive therapy and acute attacks;
  • bipolar I disorder: depressive psychosis and supportive therapy to prevent recurrences in people with bipolar I disorder who have recently experienced mixed or depressive psychosis;
  • as an adjunct to medication treatment with lithium or valproic acid for the treatment of mixed or depressive psychoses with the manifestation of psychotic symptoms;
  • as an adjuvant in the use of antidepressants for severe depressive disorder. 
  • The therapy is carried out strictly under the supervision of the attending psychiatrist. Otherwise, you can aggravate the course of the pathology and provoke serious complications. 

Contraindications for use

  • under 18 years of age;

  • hypersensitivity to aripiprazole and other components of the drug.

Use with caution in patients with cardiovascular diseases (with ischemic heart disease or myocardial infarction, with heart failure and conduction disorders), cerebrovascular diseases and conditions predisposing to arterial hypotension (dehydration, hypovolemia and taking antihypertensive drugs) in connection with the possibility of orthostatic hypotension; in patients with convulsive seizures or suffering from diseases in which convulsions are possible; in patients with an increased risk of hyperthermia (for example, with intense physical exertion, overheating, taking anticholinergic drugs, with dehydration due to the ability of neuroleptics to disrupt thermoregulation); in patients with an increased risk of aspiration pneumonia due to the risk of impaired esophageal motor function and aspiration; in obese patients with a family history of diabetes.

Application during pregnancy and lactation There are no

adequate and strictly controlled clinical studies of the safety of use during pregnancy. Abilify can be used during pregnancy in cases where the potential benefit of therapy to the mother outweighs the possible risk to the fetus.

It is not known whether aripirazole is excreted in human breast milk. It is not recommended to use the drug during lactation (breastfeeding).

In experimental studies have shown that aripiprazole is excreted in milk in lactating rats.

Application for violations of liver function

Patients with hepatic insufficiency do not require dose adjustment of the drug.

Application for impaired renal function

Patients with renal insufficiency do not require dose adjustment of the drug.

Use in children

Contraindication: under 18 years of age.

Use in elderly patients

Patients over the age of 65 years do not require dose adjustment of the drug.

Special instructions

tendency to suicidal thoughts and attempts is characteristic of patients with psychosis, bipolar disorder and major depressive disorder, therefore, drug therapy should be combined with careful medical supervision. Abilify should be prescribed in the minimum effective dose; this will reduce the risk of overdose.

The risk of developing tardive dyskinesia increases as the duration of therapy with antipsychotics increases, therefore, if symptoms of tardive dyskinesia appear while taking Abilify, the dose should be reduced or the drug canceled. After discontinuation of therapy, these symptoms may temporarily worsen or even appear for the first time.

When treating with antipsychotics, incl. aripiprazole may develop ZNS, which is manifested by hyperpyrexia, muscle rigidity, mental disorders and instability of the autonomic nervous system (irregular pulse and blood pressure, tachycardia, sweating, arrhythmia). In addition, an increase in CPK activity, myoglobinuria (rhabdomyolysis) and acute renal failure sometimes occur. In the event of symptoms of NNS or unexplained fever, all antipsychotics, incl. Abilify should be canceled.

Like other antipsychotics, Abilify should be used with caution in patients with a history of seizures and at risk of developing them.

In patients with psychoses caused by senile dementia, the risk of death increases when treated with atypical antipsychotics. In psychoses, in patients over 65 years of age with Alzheimer's disease, violations of the cardiovascular system were noted: heart attack, transient ischemic cerebrovascular accident, incl. with a lethal outcome. The use of the drug Abilify is not recommended for psychosis caused by senile dementia and in elderly patients with Alzheimer's disease.

Hyperglycemia, in some cases severe and accompanied by ketoacidosis, which can lead to a fatal hyperosmolar coma, has been observed in patients taking atypical antipsychotics. Although the relationship between taking atypical antipsychotics and hyperglycemic-type disorders remains unclear, patients diagnosed with diabetes should regularly measure blood glucose levels while taking atypical antipsychotics. Patients who have risk factors for diabetes mellitus (obesity, diabetes in a family history), when taking atypical antipsychotics, should determine the blood glucose level at the beginning of the course and periodically during the course of taking the drug. In patients taking atypical antipsychotics, constant monitoring of the symptoms of hyperglycemia (increased thirst, frequent urination, polyphagia, weakness) is necessary. Particular attention should be paid to patients with diabetes mellitus and risk factors for its development.

Due to the risk of orthostatic hypotension, Abilify should be used with caution in patients with cardiovascular diseases (myocardial infarction, coronary artery disease, heart failure, a history of cardiac conduction disorders), cerebrovascular accidents or conditions predisposing to arterial hypotension (dehydration, hypovolemia, antihypertensive therapy).

With the use of antipsychotics, there were cases of violations of the peristalsis of the esophagus and, as a result, aspiration pneumonia. The drug should be prescribed with caution to patients with risk factors for the development of aspiration pneumonia.

Influence on the ability to drive vehicles and control mechanisms

As with the use of other antipsychotics, when prescribing Abilifay, the patient should be warned about the dangers of working with moving mechanisms and driving.

Overdose

In clinical studies, accidental or intentional overdose of aripiprazole with a single dose of up to 1260 mg, not accompanied by death, has been described. Symptoms: lethargy, increased blood pressure, drowsiness, tachycardia, loss of consciousness. In hospitalized patients, no clinically significant changes in the main physiological parameters, laboratory parameters and ECG were revealed.

Cases of aripiprazole overdose in children (taking up to 195 mg) have been described. Potentially dangerous symptoms of overdose are extrapyramidal disorders and transient loss of consciousness.

Treatment: monitoring of vital signs, ECG, supportive therapy, ensuring airway patency, oxygenation, effective ventilation, activated charcoal, symptomatic treatment, close medical supervision until all symptoms disappear. There are no data on the use of hemodialysis in case of aripiprazole overdose; the beneficial effect of this method is unlikely, since aripiprazole is not excreted by the kidneys unchanged and is largely bound to plasma proteins.

Drug interaction

There was no significant effect of the blocker of histamine H2-receptors famotidine, which causes a powerful inhibition of the secretion of hydrochloric acid in the stomach, on the pharmacokinetics of aripiprazole.

Various metabolic pathways of aripiprazole are known, incl. with the participation of enzymes CYP2D6 and CYP3A4. In studies in healthy volunteers, potent inhibitors of CYP2D6 (quinidine) and CYP3A4 (ketoconazole) reduced the clearance of aripiprazole when taken orally by 52% and 38%, respectively (when used simultaneously with CYP3A4 and CYP2D6 inhibitors, the dose of aripiprazole should be reduced).

Taking aripiprazole at a dose of 30 mg simultaneously with carbamazepine, a powerful inducer of CYP3A4, was accompanied by a decrease in Cmax and AUC of aripiprazole by 68% and 73%, respectively, and a decrease in Cmax and AUC of its active metabolite dehydroaripiprazole by 69% and 71%, respectively. Other powerful inducers CYP3A4 and CYP2D6 can be expected to act similarly.

Isoenzymes CYP1A1, CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19 and CYP2E1 are not involved in the metabolism of aripiprazole in vitro, and therefore it is unlikely that it interacts with drugs and other factors (for example, smoking) that can inhibit or activate these enzymes.

Simultaneous administration of lithium or valproate with aripiprazole at a dose of 30 mg 1 time / day did not have a clinically significant effect on the pharmacokinetics of aripiprazole.

In clinical trials, aripiprazole at doses of 10-30 mg / day did not significantly affect the metabolism of substrates CYP2D6 (dextromethorphan), CYP2C9 (warfarin), CYP2C19 (omeprazole, warfarin) and CYP3A4 (dextromethorphan). In addition, aripiprazole and its main metabolite, dehydroaripiprazole, did not alter metabolism with the participation of the CYP1A2 enzyme in vitro. A clinically significant effect of aripiprazole on drugs metabolized with the participation of these isoenzymes is unlikely.

With the simultaneous use of aripiprazole (10-30 mg / day) and lamotrigine (100-400 mg / day) in patients with bipolar disorder, there were no changes in the pharmacokinetics of lamotrigine, so no dose adjustment is required.

Aripiprazole had no effect on the pharmacokinetics of escitalopram and venlafaxine in healthy volunteers; therefore, dose adjustment of these drugs is not required when administered concomitantly with aripiprazole.

When aripiprazole was used in patients with major depressive disorder simultaneously with fluoxetine (20-40 mg / day), paroxetine (37.5-50 mg / day) and sertraline (2-20 mg / day), no significant changes in plasma concentrations of antidepressants were detected.


Side effect

Determination of the frequency of side effects: very often (≥10%), often (≥1% and <10%), sometimes (≥0.1% and <1%), rarely (≥ 0.01% and <0.1%), very rarely (≤ 0.01%).

From the side of the cardiovascular system: often - orthostatic hypotension, tachycardia; sometimes - bradycardia, palpitations, myocardial infarction, prolongation of the QT interval, cardiac arrest, hemorrhage, atrial fibrillation, heart failure, AV block, myocardial ischemia, deep vein thrombosis, phlebitis, extrasystole; rarely - vasovagal syndrome, atrial flutter, thrombophlebitis, intracranial bleeding, cerebral ischemia; very rarely - fainting, increased blood pressure.

From the digestive system: very often - nausea, loss of appetite; often - increased appetite (in the treatment of depression in combination with antidepressants), dyspepsia, vomiting, constipation, salivary hypersecretion, dry mouth, heaviness in the abdomen, diarrhea; sometimes - gastroenteritis, difficulty swallowing, flatulence, gastritis, dental caries, gingivitis, hemorrhoids, gastroesophageal reflux, gastrointestinal hemorrhages, periodontal abscess, tongue edema, fecal incontinence, colitis, rectal hemorrhages, stomatitis, ulceration, mucous membrane cholecystitis, fecaloma, oral mucosa candidiasis, belching, stomach ulcer; rarely - esophagitis, bleeding gums, tongue inflammation, bloody vomiting, intestinal bleeding, duodenal ulcer, cheilitis, enlarged liver, intestinal perforation; very rarely - an increase in the activity of ALT, AST and ALP, hepatitis, jaundice, pancreatitis, dysphagia.

From the musculoskeletal system: often - arthralgia, muscle stiffness; sometimes - myasthenia gravis, arthritis, arthrosis, muscle weakness, muscle spasms, bursitis; very rarely - an increase in CPK activity, rhabdomyolysis, tendinitis, tenobursitis, myalgia.

From the side of the central nervous system and peripheral nervous system: very often - insomnia, headache, akathisia (in patients with bipolar disorder and in the treatment of depression in combination with antidepressants); often - drowsiness, dizziness, tremors, extrapyramidal syndrome, psychomotor agitation, depression, nervousness, hostility, suicidal thoughts, manic thoughts, confusion, resistance to passive movements (cogwheel syndrome), lethargy, decreased concentration, sedation; sometimes - dystonia, muscle twitching, paresthesia, limb tremor, impotence, bradykinesia, decreased / increased libido, panic reactions, apathy, memory impairment, stupor, amnesia, stroke, hyperactivity, depersonalization, dyskinesia, restless legs syndrome, myoclonus, suppressed mood, increased reflexes, slowing down of mental function, increased sensitivity to stimuli, impaired oculomotor reaction; rarely - delirium, euphoria, buccoglossal syndrome, akinesia, depression of consciousness up to loss of consciousness, decreased reflexes, obsessive thoughts, NNS; very rarely - speech disorder, convulsions.

From the respiratory system: often - shortness of breath, pneumonia; sometimes - nosebleeds, hiccups, laryngitis; rarely - hemoptysis, increased sputum production, dryness of the nasal mucosa, pulmonary edema, pulmonary embolism, hypoxia, respiratory failure, apnea.

From the senses: often - blurred vision, photophobia, ear pain; sometimes - dry eyes, eye pain, ringing in the ears, otitis media, cataracts, loss of taste, blepharitis; rarely - increased lacrimation, frequent blinking, otitis externa, amblyopia, deafness, diplopia, intraocular hemorrhage.

From the urinary system: sometimes - cystitis, frequent urination, leucorrhea, hematuria, dysuria, renal failure, albuminuria, kidney stones, nocturia, polyuria, urge to urinate; rarely - burning sensation in the urethra; very rarely - urinary incontinence, urinary retention.

From the reproductive system: sometimes - amenorrhea, premature ejaculation, vaginal bleeding, vaginal candidiasis, uterine bleeding, menorrhagia; rarely - pain in the mammary gland, cervicitis, galactorrhea, anorgasmia, burning sensation in the external genital area, gynecomastia (enlargement of the mammary glands in men), painful erection; very rarely - priapism.

From the side of metabolism: often - a decrease in body weight; sometimes - dehydration, edema, hypercholesterolemia, hypokalemia, hyperlipidemia, hypoglycemia, thirst, increased blood urea, iron deficiency anemia, increased LDH levels, obesity; rarely - hyperkalemia, gout, hypernatremia, glucosuria, cyanosis, acidification of urine; very rarely - hyponatremia, hyperglycemia, diabetic ketoacidosis, diabetic hyperosmolar coma.

Dermatological reactions: often - dry skin, itching, skin ulceration; sometimes - acne, vesiculobular (blistering) rash, eczema, alopecia, psoriasis, seborrhea; rarely - maculopapular rash, exfoliative dermatitis, hyperhidrosis.

Allergic reactions: very rarely - anaphylaxis, angioedema, pruritus, urticaria, laryngospasm.

From the side of the body as a whole: often - asthenia, fatigue, flu-like syndrome, a feeling of trembling in the body; sometimes - peripheral edema, facial edema, malaise, photosensitivity, jaw pain, chills, jaw stiffness, chest tension; rarely - sore throat, stiffness in the back, heaviness in the head, candidiasis, stiffness in the throat, Mendelssohn's syndrome, heatstroke; very rarely - violations of temperature regulation, pyrexia, pain in the chest, neck.